Article
Discovery of FYJ-195 as a Highly Potent FLT3 Inhibitor against Multiple Acquired Resistance Mutations in Acute Myeloid Leukemia.
Journal of medicinal chemistry - 11 Jun 2026
Yang Jin, Zhang Ling-Yu, Ni Xing-Feng, Bai Ming-Yu, Wang Xu, Fu An-Qi, Chen Min-Hui, Zhang Meng-Yuan, Qiao Nuo, Wang Zi-Xuan, Li Qing-Qing, Cai Shu, Wang Ying, Yao Yu-Sheng, Yu Yan-Cheng, Chen Wei-Dong, Sun Shan-Liang, Zhang Zhang, Li Nian-Guang, Shi Zhi-Hao
Abstract excerpt
The efficacy of FLT3 inhibitors in acute myeloid leukemia (AML) is severely limited by resistance mutations, particularly the recalcitrant gatekeeper F691L and activation loop D835V/Y variants. Herein, through the structure-guided optimization of our previously reported lead SILA-123, we identified FYJ-195, a highly potent type II FLT3 inhibitor capable of overcoming these recalcitrant mutants. FYJ-195 exhibited...
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